CPI-455 is a potent and selective inhibitor of KDM5 demethylases which reduces survival of drug-tolerant cancer cells. CPI-455 mediated KDM5 inhibition, elevated global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. Pretreatment of cancer cells with a KDM5-specific inhibitor results in the ablation of a subpopulation of cancer cells that can serve as the founders for therapeutic relapse.
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Name | CPI-455 HCl |
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Iupac Chemical Name | 6-isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride |
Synonyms | CPI-455 HCl; CPI-455; CPI455; CPI 455 |
Molecular Formula | C16H15ClN4O |
Molecular Weight | 314.77 |
Smile | N#CC1=C(N2N=C1)NC(C3=CC=CC=C3)=C(C2=O)C(C)C.[H]Cl |
InChiKey | OMMDFEFIJLIEDY-UHFFFAOYSA-N |
InChi | InChI=1S/C16H14N4O.ClH/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21;/h3-7,9-10,19H,1-2H3;1H |
CAS Number | 2095432-28-1 |
Related CAS |
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Formulation | Off-white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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1: Vinogradova M, Gehling VS, Gustafson A, Arora S, Tindell CA, Wilson C, Williamson KE, Guler GD, Gangurde P, Manieri W, Busby J, Flynn EM, Lan F, Kim HJ, Odate S, Cochran AG, Liu Y, Wongchenko M, Yang Y, Cheung TK, Maile TM, Lau T, Costa M, Hegde GV, Jackson E, Pitti R, Arnott D, Bailey C, Bellon S, Cummings RT, Albrecht BK, Harmange JC, Kiefer JR, Trojer P, Classon M. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8. doi: 10.1038/nchembio.2085. PubMed PMID: 27214401.